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Updated: Jul 20, 2025
Exploring the Arginine Methylome by Nuclear Magnetic Resonance Spectroscopy
Published on: December 16, 2021
CARM1 arginine methyltransferase as a therapeutic target for cancer
Margarida Santos1, Jee Won Hwang1, Mark T Bedford1
1Department of Epigenetics & Molecular Carcinogenesis, The University of Texas MD Anderson Cancer Center, Houston, Texas, USA.
Abstract:
Coactivator-associated arginine methyltransferase 1 (CARM1) is an arginine methyltransferase that posttranslationally modifies proteins that regulate multiple levels of RNA production and processing. Its substrates include histones, transcription factors, coregulators of transcription, and splicing factors. CARM1 is overexpressed in many different cancer types, and often promotes transcription factor programs that are co-opted as drivers of the transformed cell state, a process known as transcription factor addiction. Targeting these oncogenic transcription factor pathways is difficult but could be addressed by removing the activity of the key coactivators on which they rely. CARM1 is ubiquitously expressed, and its KO is less detrimental in embryonic development than deletion of the arginine methyltransferases protein arginine methyltransferase 1 and protein arginine methyltransferase 5, suggesting that therapeutic targeting of CARM1 may be well tolerated. Here, we will summarize the normal in vivo functions of CARM1 that have been gleaned from mouse studies, expand on the transcriptional pathways that are regulated by CARM1, and finally highlight recent studies that have identified oncogenic properties of CARM1 in different biological settings. This review is meant to kindle an interest in the development of human drug therapies targeting CARM1, as there are currently no CARM1 inhibitors available for use in clinical trials.
Insights
Coactivator-associated arginine methyltransferase 1 (CARM1) is an enzyme overexpressed in many cancers. Targeting CARM1 may offer a well-tolerated therapeutic strategy for cancer by disrupting oncogenic transcription factor pathways.
Area of Science:
- Molecular Biology
- Epigenetics
- Cancer Biology
Background:
- Coactivator-associated arginine methyltransferase 1 (CARM1) is an enzyme that modifies proteins involved in RNA production and processing.
- CARM1 substrates include histones, transcription factors, and splicing factors, playing roles in gene regulation.
- Overexpression of CARM1 is observed in numerous cancer types, contributing to transcription factor addiction.
Purpose of the Study:
- To review the in vivo functions of CARM1 based on mouse studies.
- To elaborate on the transcriptional pathways regulated by CARM1.
- To highlight recent findings on the oncogenic properties of CARM1 and its therapeutic potential.
Main Methods:
- Literature review of studies on CARM1 function in vivo, particularly in mouse models.
- Analysis of research identifying CARM1's role in transcriptional regulation.
- Synthesis of recent findings linking CARM1 to oncogenesis.
Main Results:
- CARM1 plays a role in RNA production, processing, and epigenetic regulation.
- CARM1 is implicated in promoting transcription factor programs that drive cancer cell transformation.
- CARM1 knockout is less detrimental to embryonic development compared to other related enzymes, suggesting potential therapeutic tolerability.
Conclusions:
- CARM1 is a promising therapeutic target for various cancers due to its role in oncogenic pathways.
- Further research into CARM1 inhibitors could lead to novel cancer treatments.
- Targeting CARM1 may be a viable strategy to address transcription factor addiction in cancer.
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